RU2007137669A - APPLICATION OF COMPOUND - Google Patents
APPLICATION OF COMPOUND Download PDFInfo
- Publication number
- RU2007137669A RU2007137669A RU2007137669/15A RU2007137669A RU2007137669A RU 2007137669 A RU2007137669 A RU 2007137669A RU 2007137669/15 A RU2007137669/15 A RU 2007137669/15A RU 2007137669 A RU2007137669 A RU 2007137669A RU 2007137669 A RU2007137669 A RU 2007137669A
- Authority
- RU
- Russia
- Prior art keywords
- rapamycin
- use according
- desmethoxy
- analog
- treatment
- Prior art date
Links
- 150000001875 compounds Chemical class 0.000 title 1
- 239000003814 drug Substances 0.000 claims abstract 17
- DIEORUOOFDNDCG-UHFFFAOYSA-N 41-desmethoxyrapamycin 31-OTMS Natural products C1C(=O)C(C)C=C(C)C(O)C(OC)C(=O)C(C)CC(C)C=CC=CC=C(C)C(OC)CC(O2)CCC(C)C2(O)C(=O)C(=O)N2CCCCC2C(=O)OC1C(C)CC1CCC(O)CC1 DIEORUOOFDNDCG-UHFFFAOYSA-N 0.000 claims abstract 16
- 229910052739 hydrogen Inorganic materials 0.000 claims abstract 15
- 206010028980 Neoplasm Diseases 0.000 claims abstract 9
- 230000000626 neurodegenerative effect Effects 0.000 claims abstract 8
- 230000001575 pathological effect Effects 0.000 claims abstract 8
- 208000012526 B-cell neoplasm Diseases 0.000 claims abstract 6
- 229940079593 drug Drugs 0.000 claims abstract 6
- 150000003839 salts Chemical class 0.000 claims abstract 6
- 208000003174 Brain Neoplasms Diseases 0.000 claims abstract 4
- 238000004519 manufacturing process Methods 0.000 claims abstract 4
- 208000024827 Alzheimer disease Diseases 0.000 claims abstract 2
- 201000010915 Glioblastoma multiforme Diseases 0.000 claims abstract 2
- 208000027418 Wounds and injury Diseases 0.000 claims abstract 2
- 230000008499 blood brain barrier function Effects 0.000 claims abstract 2
- 210000001218 blood-brain barrier Anatomy 0.000 claims abstract 2
- 210000004556 brain Anatomy 0.000 claims abstract 2
- 210000003169 central nervous system Anatomy 0.000 claims abstract 2
- 230000006378 damage Effects 0.000 claims abstract 2
- 201000010099 disease Diseases 0.000 claims abstract 2
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims abstract 2
- 208000005017 glioblastoma Diseases 0.000 claims abstract 2
- 208000014674 injury Diseases 0.000 claims abstract 2
- 201000006417 multiple sclerosis Diseases 0.000 claims abstract 2
- 230000001537 neural effect Effects 0.000 claims abstract 2
- 210000004881 tumor cell Anatomy 0.000 claims abstract 2
- AOJJSUZBOXZQNB-TZSSRYMLSA-N Doxorubicin Chemical compound O([C@H]1C[C@@](O)(CC=2C(O)=C3C(=O)C=4C=CC=C(C=4C(=O)C3=C(O)C=21)OC)C(=O)CO)[C@H]1C[C@H](N)[C@H](O)[C@H](C)O1 AOJJSUZBOXZQNB-TZSSRYMLSA-N 0.000 claims 4
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 4
- ZAHRKKWIAAJSAO-UHFFFAOYSA-N rapamycin Natural products COCC(O)C(=C/C(C)C(=O)CC(OC(=O)C1CCCCN1C(=O)C(=O)C2(O)OC(CC(OC)C(=CC=CC=CC(C)CC(C)C(=O)C)C)CCC2C)C(C)CC3CCC(O)C(C3)OC)C ZAHRKKWIAAJSAO-UHFFFAOYSA-N 0.000 claims 3
- QFJCIRLUMZQUOT-HPLJOQBZSA-N sirolimus Chemical compound C1C[C@@H](O)[C@H](OC)C[C@@H]1C[C@@H](C)[C@H]1OC(=O)[C@@H]2CCCCN2C(=O)C(=O)[C@](O)(O2)[C@H](C)CC[C@H]2C[C@H](OC)/C(C)=C/C=C/C=C/[C@@H](C)C[C@@H](C)C(=O)[C@H](OC)[C@H](O)/C(C)=C/[C@@H](C)C(=O)C1 QFJCIRLUMZQUOT-HPLJOQBZSA-N 0.000 claims 3
- 229960002930 sirolimus Drugs 0.000 claims 3
- 102100033350 ATP-dependent translocase ABCB1 Human genes 0.000 claims 2
- 108010047230 Member 1 Subfamily B ATP Binding Cassette Transporter Proteins 0.000 claims 2
- NKANXQFJJICGDU-QPLCGJKRSA-N Tamoxifen Chemical compound C=1C=CC=CC=1C(/CC)=C(C=1C=CC(OCCN(C)C)=CC=1)/C1=CC=CC=C1 NKANXQFJJICGDU-QPLCGJKRSA-N 0.000 claims 2
- 239000008194 pharmaceutical composition Substances 0.000 claims 2
- VVIAGPKUTFNRDU-UHFFFAOYSA-N 6S-folinic acid Natural products C1NC=2NC(N)=NC(=O)C=2N(C=O)C1CNC1=CC=C(C(=O)NC(CCC(O)=O)C(O)=O)C=C1 VVIAGPKUTFNRDU-UHFFFAOYSA-N 0.000 claims 1
- 108010006654 Bleomycin Proteins 0.000 claims 1
- GAGWJHPBXLXJQN-UORFTKCHSA-N Capecitabine Chemical compound C1=C(F)C(NC(=O)OCCCCC)=NC(=O)N1[C@H]1[C@H](O)[C@H](O)[C@@H](C)O1 GAGWJHPBXLXJQN-UORFTKCHSA-N 0.000 claims 1
- GAGWJHPBXLXJQN-UHFFFAOYSA-N Capecitabine Natural products C1=C(F)C(NC(=O)OCCCCC)=NC(=O)N1C1C(O)C(O)C(C)O1 GAGWJHPBXLXJQN-UHFFFAOYSA-N 0.000 claims 1
- CMSMOCZEIVJLDB-UHFFFAOYSA-N Cyclophosphamide Chemical compound ClCCN(CCCl)P1(=O)NCCCO1 CMSMOCZEIVJLDB-UHFFFAOYSA-N 0.000 claims 1
- 102000009024 Epidermal Growth Factor Human genes 0.000 claims 1
- 101800003838 Epidermal growth factor Proteins 0.000 claims 1
- GHASVSINZRGABV-UHFFFAOYSA-N Fluorouracil Chemical compound FC1=CNC(=O)NC1=O GHASVSINZRGABV-UHFFFAOYSA-N 0.000 claims 1
- BLCLNMBMMGCOAS-URPVMXJPSA-N Goserelin Chemical compound C([C@@H](C(=O)N[C@H](COC(C)(C)C)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N1[C@@H](CCC1)C(=O)NNC(N)=O)NC(=O)[C@H](CO)NC(=O)[C@H](CC=1C2=CC=CC=C2NC=1)NC(=O)[C@H](CC=1NC=NC=1)NC(=O)[C@H]1NC(=O)CC1)C1=CC=C(O)C=C1 BLCLNMBMMGCOAS-URPVMXJPSA-N 0.000 claims 1
- 108010069236 Goserelin Proteins 0.000 claims 1
- VEXZGXHMUGYJMC-UHFFFAOYSA-N Hydrochloric acid Chemical compound Cl VEXZGXHMUGYJMC-UHFFFAOYSA-N 0.000 claims 1
- HEFNNWSXXWATRW-UHFFFAOYSA-N Ibuprofen Chemical compound CC(C)CC1=CC=C(C(C)C(O)=O)C=C1 HEFNNWSXXWATRW-UHFFFAOYSA-N 0.000 claims 1
- FBOZXECLQNJBKD-ZDUSSCGKSA-N L-methotrexate Chemical compound C=1N=C2N=C(N)N=C(N)C2=NC=1CN(C)C1=CC=C(C(=O)N[C@@H](CCC(O)=O)C(O)=O)C=C1 FBOZXECLQNJBKD-ZDUSSCGKSA-N 0.000 claims 1
- ZDZOTLJHXYCWBA-VCVYQWHSSA-N N-debenzoyl-N-(tert-butoxycarbonyl)-10-deacetyltaxol Chemical compound O([C@H]1[C@H]2[C@@](C([C@H](O)C3=C(C)[C@@H](OC(=O)[C@H](O)[C@@H](NC(=O)OC(C)(C)C)C=4C=CC=CC=4)C[C@]1(O)C3(C)C)=O)(C)[C@@H](O)C[C@H]1OC[C@]12OC(=O)C)C(=O)C1=CC=CC=C1 ZDZOTLJHXYCWBA-VCVYQWHSSA-N 0.000 claims 1
- 229930012538 Paclitaxel Natural products 0.000 claims 1
- 229940079156 Proteasome inhibitor Drugs 0.000 claims 1
- 108010073929 Vascular Endothelial Growth Factor A Proteins 0.000 claims 1
- 102000005789 Vascular Endothelial Growth Factors Human genes 0.000 claims 1
- 108010019530 Vascular Endothelial Growth Factors Proteins 0.000 claims 1
- JXLYSJRDGCGARV-WWYNWVTFSA-N Vinblastine Natural products O=C(O[C@H]1[C@](O)(C(=O)OC)[C@@H]2N(C)c3c(cc(c(OC)c3)[C@]3(C(=O)OC)c4[nH]c5c(c4CCN4C[C@](O)(CC)C[C@H](C3)C4)cccc5)[C@@]32[C@H]2[C@@]1(CC)C=CCN2CC3)C JXLYSJRDGCGARV-WWYNWVTFSA-N 0.000 claims 1
- 229940009456 adriamycin Drugs 0.000 claims 1
- YBBLVLTVTVSKRW-UHFFFAOYSA-N anastrozole Chemical compound N#CC(C)(C)C1=CC(C(C)(C#N)C)=CC(CN2N=CN=C2)=C1 YBBLVLTVTVSKRW-UHFFFAOYSA-N 0.000 claims 1
- 229960002932 anastrozole Drugs 0.000 claims 1
- 239000002246 antineoplastic agent Substances 0.000 claims 1
- 229960001561 bleomycin Drugs 0.000 claims 1
- OYVAGSVQBOHSSS-UAPAGMARSA-O bleomycin A2 Chemical compound N([C@H](C(=O)N[C@H](C)[C@@H](O)[C@H](C)C(=O)N[C@@H]([C@H](O)C)C(=O)NCCC=1SC=C(N=1)C=1SC=C(N=1)C(=O)NCCC[S+](C)C)[C@@H](O[C@H]1[C@H]([C@@H](O)[C@H](O)[C@H](CO)O1)O[C@@H]1[C@H]([C@@H](OC(N)=O)[C@H](O)[C@@H](CO)O1)O)C=1N=CNC=1)C(=O)C1=NC([C@H](CC(N)=O)NC[C@H](N)C(N)=O)=NC(N)=C1C OYVAGSVQBOHSSS-UAPAGMARSA-O 0.000 claims 1
- 229960004117 capecitabine Drugs 0.000 claims 1
- 239000003795 chemical substances by application Substances 0.000 claims 1
- 229960004397 cyclophosphamide Drugs 0.000 claims 1
- 229960003668 docetaxel Drugs 0.000 claims 1
- 229960004679 doxorubicin Drugs 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 229940116977 epidermal growth factor Drugs 0.000 claims 1
- 229960002949 fluorouracil Drugs 0.000 claims 1
- VVIAGPKUTFNRDU-ABLWVSNPSA-N folinic acid Chemical compound C1NC=2NC(N)=NC(=O)C=2N(C=O)C1CNC1=CC=C(C(=O)N[C@@H](CCC(O)=O)C(O)=O)C=C1 VVIAGPKUTFNRDU-ABLWVSNPSA-N 0.000 claims 1
- 235000008191 folinic acid Nutrition 0.000 claims 1
- 239000011672 folinic acid Substances 0.000 claims 1
- 229960002913 goserelin Drugs 0.000 claims 1
- 239000003481 heat shock protein 90 inhibitor Substances 0.000 claims 1
- 229940022353 herceptin Drugs 0.000 claims 1
- 239000001257 hydrogen Substances 0.000 claims 1
- 125000004435 hydrogen atom Chemical group [H]* 0.000 claims 1
- 239000003112 inhibitor Substances 0.000 claims 1
- 238000001990 intravenous administration Methods 0.000 claims 1
- 229960001691 leucovorin Drugs 0.000 claims 1
- RQZAXGRLVPAYTJ-GQFGMJRRSA-N megestrol acetate Chemical compound C1=C(C)C2=CC(=O)CC[C@]2(C)[C@@H]2[C@@H]1[C@@H]1CC[C@@](C(C)=O)(OC(=O)C)[C@@]1(C)CC2 RQZAXGRLVPAYTJ-GQFGMJRRSA-N 0.000 claims 1
- 229960004296 megestrol acetate Drugs 0.000 claims 1
- 229960000485 methotrexate Drugs 0.000 claims 1
- 229960001592 paclitaxel Drugs 0.000 claims 1
- -1 prenizone Chemical compound 0.000 claims 1
- 239000003207 proteasome inhibitor Substances 0.000 claims 1
- 108091006082 receptor inhibitors Proteins 0.000 claims 1
- 229960001603 tamoxifen Drugs 0.000 claims 1
- RCINICONZNJXQF-MZXODVADSA-N taxol Chemical compound O([C@@H]1[C@@]2(C[C@@H](C(C)=C(C2(C)C)[C@H](C([C@]2(C)[C@@H](O)C[C@H]3OC[C@]3([C@H]21)OC(C)=O)=O)OC(=O)C)OC(=O)[C@H](O)[C@@H](NC(=O)C=1C=CC=CC=1)C=1C=CC=CC=1)O)C(=O)C1=CC=CC=C1 RCINICONZNJXQF-MZXODVADSA-N 0.000 claims 1
- XFCLJVABOIYOMF-QPLCGJKRSA-N toremifene Chemical compound C1=CC(OCCN(C)C)=CC=C1C(\C=1C=CC=CC=1)=C(\CCCl)C1=CC=CC=C1 XFCLJVABOIYOMF-QPLCGJKRSA-N 0.000 claims 1
- 229960005026 toremifene Drugs 0.000 claims 1
- VBEQCZHXXJYVRD-GACYYNSASA-N uroanthelone Chemical compound C([C@@H](C(=O)N[C@H](C(=O)N[C@@H](CS)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CS)C(=O)N[C@H](C(=O)N[C@@H]([C@@H](C)CC)C(=O)NCC(=O)N[C@@H](CC=1C=CC(O)=CC=1)C(=O)N[C@@H](CO)C(=O)NCC(=O)N[C@@H](CC(O)=O)C(=O)N[C@@H](CCCNC(N)=N)C(=O)N[C@@H](CS)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H]([C@@H](C)O)C(=O)N[C@@H](CCCNC(N)=N)C(=O)N[C@@H](CC(O)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(N)=N)C(=O)N[C@@H](CC=1C2=CC=CC=C2NC=1)C(=O)N[C@@H](CC=1C2=CC=CC=C2NC=1)C(=O)N[C@@H](CCC(O)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(N)=N)C(O)=O)C(C)C)[C@@H](C)O)NC(=O)[C@H](CO)NC(=O)[C@H](CC(O)=O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CO)NC(=O)[C@H](CCC(O)=O)NC(=O)[C@@H](NC(=O)[C@H](CC=1NC=NC=1)NC(=O)[C@H](CCSC)NC(=O)[C@H](CS)NC(=O)[C@@H](NC(=O)CNC(=O)CNC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CS)NC(=O)[C@H](CC=1C=CC(O)=CC=1)NC(=O)CNC(=O)[C@H](CC(O)=O)NC(=O)[C@H](CC=1C=CC(O)=CC=1)NC(=O)[C@H](CO)NC(=O)[C@H](CO)NC(=O)[C@H]1N(CCC1)C(=O)[C@H](CS)NC(=O)CNC(=O)[C@H]1N(CCC1)C(=O)[C@H](CC=1C=CC(O)=CC=1)NC(=O)[C@H](CO)NC(=O)[C@@H](N)CC(N)=O)C(C)C)[C@@H](C)CC)C1=CC=C(O)C=C1 VBEQCZHXXJYVRD-GACYYNSASA-N 0.000 claims 1
- 229960003048 vinblastine Drugs 0.000 claims 1
- JXLYSJRDGCGARV-XQKSVPLYSA-N vincaleukoblastine Chemical compound C([C@@H](C[C@]1(C(=O)OC)C=2C(=CC3=C([C@]45[C@H]([C@@]([C@H](OC(C)=O)[C@]6(CC)C=CCN([C@H]56)CC4)(O)C(=O)OC)N3C)C=2)OC)C[C@@](C2)(O)CC)N2CCC2=C1NC1=CC=CC=C21 JXLYSJRDGCGARV-XQKSVPLYSA-N 0.000 claims 1
- 229960004528 vincristine Drugs 0.000 claims 1
- OGWKCGZFUXNPDA-XQKSVPLYSA-N vincristine Chemical compound C([N@]1C[C@@H](C[C@]2(C(=O)OC)C=3C(=CC4=C([C@]56[C@H]([C@@]([C@H](OC(C)=O)[C@]7(CC)C=CCN([C@H]67)CC5)(O)C(=O)OC)N4C=O)C=3)OC)C[C@@](C1)(O)CC)CC1=C2NC2=CC=CC=C12 OGWKCGZFUXNPDA-XQKSVPLYSA-N 0.000 claims 1
- OGWKCGZFUXNPDA-UHFFFAOYSA-N vincristine Natural products C1C(CC)(O)CC(CC2(C(=O)OC)C=3C(=CC4=C(C56C(C(C(OC(C)=O)C7(CC)C=CCN(C67)CC5)(O)C(=O)OC)N4C=O)C=3)OC)CN1CCC1=C2NC2=CC=CC=C12 OGWKCGZFUXNPDA-UHFFFAOYSA-N 0.000 claims 1
- GBABOYUKABKIAF-GHYRFKGUSA-N vinorelbine Chemical compound C1N(CC=2C3=CC=CC=C3NC=22)CC(CC)=C[C@H]1C[C@]2(C(=O)OC)C1=CC([C@]23[C@H]([C@]([C@H](OC(C)=O)[C@]4(CC)C=CCN([C@H]34)CC2)(O)C(=O)OC)N2C)=C2C=C1OC GBABOYUKABKIAF-GHYRFKGUSA-N 0.000 claims 1
- 229960002066 vinorelbine Drugs 0.000 claims 1
- 125000000956 methoxy group Chemical group [H]C([H])([H])O* 0.000 abstract 3
- 230000000259 anti-tumor effect Effects 0.000 abstract 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D498/12—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains three hetero rings
- C07D498/14—Ortho-condensed systems
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/47—Quinolines; Isoquinolines
- A61K31/4738—Quinolines; Isoquinolines ortho- or peri-condensed with heterocyclic ring systems
- A61K31/4745—Quinolines; Isoquinolines ortho- or peri-condensed with heterocyclic ring systems condensed with ring systems having nitrogen as a ring hetero atom, e.g. phenantrolines
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
- A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
Abstract
1. Применение аналога 39-десметоксирапамицина формулы (I), где R1 представлен (Н,Н) или =O, a R2 и R3 каждый независимо представлены Н, ОН или ОСН3; или его фармацевтически приемлемой соли, в приготовлении медикамента для лечения патологического состояния, являющего результатом нейронного повреждения или заболевания. ! ! 2. Применение аналога 39-десметоксирапамицина формулы (I), где R1 представлен (Н, Н) или =O, a R2 и R3 каждый независимо представлены Н, ОН или ОСН3, в приготовлении медикамента для лечения патологического состояния, затрагивающего центральную нервную систему, где патологическое состояние требует медикамента, пересекающего гематоэнцефалический барьер. ! ! 3. Применение по п.1 или 2, где патологическое состояние выбрано из группы, состоящей из опухоли(лей) головного мозга и нейродегенеративных состояний. ! 4. Применение по п.3, где медикамент предназначен для лечения опухолей головного мозга. ! 5. Применение по п.4, где опухолью головного мозга является мультиформная глиобластома. ! 6. Применение по п.3, где медикамент предназначен для лечения нейродегенеративных состояний. ! 7. Применение по п.6, где нейродегенеративным состоянием является болезнь Альцгеймера. ! 8. Применение по п.6, где нейродегенеративным состоянием является рассеянный склероз. ! 9. Применение аналога 39-десметоксирапамицина формулы (I), где R1 представлен (Н, Н) или =O, a R2 и R3 каждый независимо представлены Н, ОН или ОСН3; или его фармацевтически приемлемой соли, в приготовлении медикамента для лечения опухолей или В-клеточных новообразований, где опухоль или В-клеточное новообразование является резистентным к одному или более существующим противоопухолевым а�1. The use of an analog of 39-desmethoxy-rapamycin of formula (I), where R1 is (H, H) or = O, and R2 and R3 are each independently H, OH or OCH3; or a pharmaceutically acceptable salt thereof, in the manufacture of a medicament for the treatment of a pathological condition resulting from a neural injury or disease. ! ! 2. The use of an analog of 39-desmethoxy-rapamycin of formula (I), where R1 is (H, H) or = O, and R2 and R3 are each independently H, OH or OCH3, in the preparation of a medicament for the treatment of a pathological condition affecting the central nervous system, where the pathological condition requires a medication that crosses the blood-brain barrier. ! ! 3. The use according to claim 1 or 2, where the pathological condition is selected from the group consisting of tumor (s) of the brain and neurodegenerative conditions. ! 4. The use according to claim 3, where the medication is intended for the treatment of brain tumors. ! 5. The use according to claim 4, where the brain tumor is glioblastoma multiforme. ! 6. The use according to claim 3, where the medication is intended for the treatment of neurodegenerative conditions. ! 7. The use according to claim 6, where the neurodegenerative condition is Alzheimer's disease. ! 8. The use according to claim 6, where the neurodegenerative state is multiple sclerosis. ! 9. The use of an analog of 39-desmethoxy-rapamycin of the formula (I), wherein R1 is (H, H) or = O, and R2 and R3 are each independently H, OH or OCH3; or a pharmaceutically acceptable salt thereof, in the manufacture of a medicament for the treatment of tumors or B-cell neoplasms, where the tumor or B-cell neoplasm is resistant to one or more existing antitumor a
Claims (25)
Applications Claiming Priority (5)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
GB0504995.2 | 2005-03-11 | ||
GBGB0504995.2A GB0504995D0 (en) | 2005-03-11 | 2005-03-11 | Use of a compound |
US11/097,605 | 2005-04-01 | ||
US11/097,605 US7183289B2 (en) | 2005-03-11 | 2005-04-01 | 39-desmethoxyrapamycin, compositions and methods of use thereof |
GB0522829.1 | 2005-11-09 |
Publications (2)
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RU2007137669A true RU2007137669A (en) | 2009-04-20 |
RU2428982C2 RU2428982C2 (en) | 2011-09-20 |
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RU2007137669/15A RU2428982C2 (en) | 2005-03-11 | 2006-03-10 | Application of compound |
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US (2) | US7183289B2 (en) |
CN (1) | CN101180054A (en) |
GB (1) | GB0504995D0 (en) |
RU (1) | RU2428982C2 (en) |
UA (1) | UA94580C2 (en) |
Families Citing this family (19)
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US7585517B2 (en) * | 2003-09-18 | 2009-09-08 | Macusight, Inc. | Transscleral delivery |
BRPI0607606B1 (en) * | 2005-02-09 | 2021-06-22 | Santen Pharmaceutical, Co., Ltd. | LIQUID FORMULATION |
US8663639B2 (en) * | 2005-02-09 | 2014-03-04 | Santen Pharmaceutical Co., Ltd. | Formulations for treating ocular diseases and conditions |
US20100061994A1 (en) * | 2005-03-11 | 2010-03-11 | Rose Mary Sheridan | Medical uses of 39-desmethoxyrapamycin and analogues thereof |
GB0504994D0 (en) * | 2005-03-11 | 2005-04-20 | Biotica Tech Ltd | Novel compounds |
EP2001438A2 (en) | 2006-02-09 | 2008-12-17 | Macusight, Inc. | Stable formulations, and methods of their preparation and use |
JP5506378B2 (en) | 2006-03-23 | 2014-05-28 | 参天製薬株式会社 | Formulations and methods for diseases or conditions associated with vascular permeability |
GB0618403D0 (en) * | 2006-09-19 | 2006-11-01 | Leuven K U Res & Dev | Treatment of amyotrophic lateral sclerosis |
MX2009010683A (en) * | 2007-04-05 | 2010-01-20 | Wyeth Corp | Wortmannin-rapamycin conjugate and uses thereof. |
TW200845960A (en) * | 2007-04-05 | 2008-12-01 | Wyeth Corp | Wortmannin-rapalog conjugate and uses thereof |
US20080265343A1 (en) * | 2007-04-26 | 2008-10-30 | International Business Machines Corporation | Field effect transistor with inverted t shaped gate electrode and methods for fabrication thereof |
US8754094B2 (en) * | 2007-08-15 | 2014-06-17 | The Research Foundation Of State University Of New York | Methods for heat shock protein dependent cancer treatment |
WO2009105230A2 (en) * | 2008-02-21 | 2009-08-27 | The Regents Of The University Of Colorado | Methods for treating cancer using combination therapy |
GB201122305D0 (en) * | 2011-12-23 | 2012-02-01 | Biotica Tech Ltd | Novel compound |
EP3024457A4 (en) | 2013-07-26 | 2017-06-28 | Update Pharma Inc. | Compositions to improve the therapeutic benefit of bisantrene |
WO2019157382A1 (en) * | 2018-02-09 | 2019-08-15 | Mount Tam Therapeutics, Inc. | Rapamycin analog for prevention and/or treatment of neurodegenerative conditions |
US11633399B2 (en) | 2018-12-25 | 2023-04-25 | Sol-Gel Technologies Ltd. | Treatment of skin disorders with compositions comprising an EGFR inhibitor |
CN111007161B (en) * | 2019-11-04 | 2021-03-26 | 中南大学 | Peptide fragment composition for predicting drug effect of methotrexate, quantitative detection method and detection kit thereof |
WO2022179575A1 (en) * | 2021-02-25 | 2022-09-01 | 中以海德人工智能药物研发股份有限公司 | Application of rapamycin in treatment or prevention of hepatitis b |
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US5708002A (en) * | 1991-09-05 | 1998-01-13 | Abbott Laboratories | Macrocyclic immunomodulators |
JP3140228B2 (en) | 1992-02-17 | 2001-03-05 | ファイザー製薬株式会社 | Novel macrocyclic lactone and its producing bacteria |
GB9315914D0 (en) * | 1993-07-31 | 1993-09-15 | Smithkline Beecham Plc | Novel compound |
EP0937082A2 (en) | 1996-07-12 | 1999-08-25 | Ariad Pharmaceuticals, Inc. | Materials and method for treating or preventing pathogenic fungal infection |
US6273913B1 (en) * | 1997-04-18 | 2001-08-14 | Cordis Corporation | Modified stent useful for delivery of drugs along stent strut |
US6485514B1 (en) * | 1997-12-12 | 2002-11-26 | Supergen, Inc. | Local delivery of therapeutic agents |
CA2994779C (en) * | 2001-02-19 | 2020-08-25 | Novartis Ag | Use of 40-o-(2-hydroxyethyl)-rapamycin for inhibiting growth of a solid tumour of the brain other than lymphatic cancer |
EP1478648B1 (en) * | 2002-02-01 | 2014-04-30 | ARIAD Pharmaceuticals, Inc. | Phosphorus-containing compounds and uses thereof |
EP1967520A2 (en) | 2002-07-16 | 2008-09-10 | Biotica Technology Limited | Production of polyketides and other natural products |
EP1896018A2 (en) * | 2005-03-11 | 2008-03-12 | Biotica Technology Limited | Medical uses of 39-desmethoxyrapamycin and analogues thereof |
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2005
- 2005-03-11 GB GBGB0504995.2A patent/GB0504995D0/en not_active Ceased
- 2005-04-01 US US11/097,605 patent/US7183289B2/en not_active Expired - Fee Related
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2006
- 2006-03-10 RU RU2007137669/15A patent/RU2428982C2/en not_active IP Right Cessation
- 2006-03-10 CN CNA2006800126751A patent/CN101180054A/en active Pending
- 2006-10-03 UA UAA200711241A patent/UA94580C2/en unknown
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2007
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US7183289B2 (en) | 2007-02-27 |
US7655673B2 (en) | 2010-02-02 |
RU2428982C2 (en) | 2011-09-20 |
US20070184075A1 (en) | 2007-08-09 |
CN101180054A (en) | 2008-05-14 |
US20060205757A1 (en) | 2006-09-14 |
UA94580C2 (en) | 2011-05-25 |
GB0504995D0 (en) | 2005-04-20 |
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